Convenient methods are reported for the synthesis of 1,4-disubstituted and 1-substituted β-carbolines from 3-substituted 2-acylindoles, which are accessible through two one-pot multistep reactions via oxomethylated benzenesulfonamide intermediates. The acylindoles are subsequently subjected to aminomethylenation with formamide derivatives or chemoselective reduction, followed by ring closure with ammonium salts.

中文翻译：

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通过 3-取代 2-酰吲哚合成 1,4-二取代和 1-取代 β-咔啉


据报道，从3-取代的2-酰吲哚合成1,4-二取代和1-取代的β-咔啉的简便方法，可以通过氧代甲基化苯磺酰胺中间体通过两个一锅多步反应来实现。随后用甲酰胺衍生物对酰吲哚进行氨甲基化或化学选择性还原，然后用铵盐进行闭环。